• 제목/요약/키워드: ${\alpha}$-Glucosidase inhibitory

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Sargassum yezoense Extract Inhibits Carbohydrate Digestive Enzymes In Vitro and Alleviates Postprandial Hyperglycemia in Diabetic Mice.

  • Park, Jae-Eun;Lee, Ji-Hee;Han, Ji-Sook
    • Preventive Nutrition and Food Science
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    • 제22권3호
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    • pp.166-171
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    • 2017
  • In this study, we investigated whether Sargassum yezoense extract (SYE) could inhibit ${\alpha}-glucosidase$ and ${\alpha}-amylase$ activities, and alleviate postprandial hyperglycemia in streptozotocin (STZ)-induced diabetic mice. Freeze-dried S. yezoense was extracted with 80% ethanol and concentrated for use in this study. The hypoglycemic effect was determined by evaluating the inhibitory activities of SYE against ${\alpha}-glucosidase$ and ${\alpha}-amylase$ as well as its ability to decrease postprandial blood glucose levels. The half-maximal inhibitory concentrations of SYE against ${\alpha}-glucosidase$ and ${\alpha}-amylase$ were $0.078{\pm}0.004$ and $0.212{\pm}0.064mg/mL$, respectively. SYE was a more effective inhibitor of ${\alpha}-glucosidase$ and ${\alpha}-amylase$ activities than the positive control, acarbose. The increase in postprandial blood glucose levels was significantly alleviated in the SYE group compared with that in the control group of STZ-induced diabetic mice. Furthermore, the area under the curves significantly decreased with SYE administration in STZ-induced diabetic mice. These results suggest that SYE is a potent inhibitor of ${\alpha}-glucosidase$ and ${\alpha}-amylase$ activities and alleviates postprandial hyperglycemia caused by dietary carbohydrates.

작약(Paeoniae radix) 추출물의 식후 과혈당 억제작용 (Inhibitory Effect of Extracts from Paeoniae radix on Postprandial Hyperglycemia)

  • 지승택;이성진;이강은;손용태;정요경
    • 한국식품영양과학회지
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    • 제31권1호
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    • pp.131-135
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    • 2002
  • 본 연구에서는 작약 추출물의 식후 과혈당 억제작용을 조사하였다. 작약 유기용매(hexane, ethyl acetate, butanol, water) 추출물들을 high performance liquid chromatogrphy를 이용하여 분획한 분획물(fraction)들으 $\alpha$-glucosidase(EC 3.2.1.20) 저해제를 탐색하였다. 작약 ethyl acetate 추출물의 11, 12, 18, 19번 분획물들은 20 $\mu\textrm{g}$/mL에서 각각 85%, 84%, 77%, 77%의 강력한 저해 활성을 나타내었으며, 작약 ethyl acetate 추출물의 10~19번 분획을 경구투여한 in vivo당 (maltose) 부하 실험에서도 양성대조군과 비교하여 유의성 있게 22%의 혈당을 낮추었다. 따라서 본 연구의 in vitro와 in vivo 실험을 통하여 확인 된 $\alpha$-glucosidase 저해 활성을 갖는 작약 분획물들은 식후의 혈당상승 작용을 억제하는 새로운 nutraceutical 소재와 항당뇨 신약개발을 위한 탐색자원으로서 매우 가치있는 자원으로 기대된다.

더덕과 일부 한약재 열수추출물의 혼합 비율에 따른 생리활성 (Physiological Functionalities of Hot Water Extract of Codonopsis lanceolata and Some Medicinal Materials, and Their Mixtures)

  • 오혜숙;김준호
    • 한국지역사회생활과학회지
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    • 제18권3호
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    • pp.407-415
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    • 2007
  • The aim of this study was to investigate the physiological functionalities of Codonopsis lanceolata, Glycyrrhiza uralensis, Chaenomeles sinensis, Crataegus pinnafida, and their mixtures. We also determined their antioxidative, fibrinolytic, and ${\alpha}-glucosidase$ inhibitory activities. The antioxidative activities of Codonopsis lanceolata, Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida were 79%, 88.3%, 89.9%, and 89.3% respectively. Their fibrinolytic activities were 0.80plasmin unit/mi, 0.57 plasmin unit/mi, 0.52 plasmin unit/mi, and 0.53 plasmin unit/mi respectively. The ${\alpha}-glucosidase$ inhibitory activity of Codonopsis lanceolata was 25%. The 10-fold diluents of Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida showed ${\alpha}-glucosidase$ inhibitory activities of 93.6%, 65.3%, and 61.3% respectively. In antioxidative activity tests of the medicinal plants mixtures at various ratios, the mixtures of Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida with Codonopsis lanceolata showed antioxidative activities of approximately 90%. In fibrinolytic activity tests mixtures(1:1) of Codonopsis lanceolata with Chaenomeles sinensis and Crataegus pinnafida exhibited increases of 23% and 24% in activity respectively. In ${\alpha}-glucosidase$ inhibitory activity tests, a mixture (4:1) of Codonopsis lanceolata and 10-fold diluted Glycyrrhiza uralensis showed an inhibitory activity of 98%, a mixture (3:1) of Codonopsis lanceolata and 10-fold diluted Chaenomeles sinensis showed an inhibitory activity of 69.6%, and a mixture (1:1) of Codonopsis lanceolata and 10-fold diluted Crataegus pinnafida showed an inhibitory activity of 50.2%. In conclusion, the mixtures of Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida with Codonopsis lanceolata will be used as a material for the development of biofunctional foods.

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Biological activities of Solvent Fractions Isolated from Areca catechu L

  • 김준호
    • 대한의생명과학회지
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    • 제16권4호
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    • pp.271-277
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    • 2010
  • This study was conducted to investigate the biological activities of Areca catechu L. The antioxidative, fibrinolytic, thrombin inhibitory, and ${\alpha}$-glucosidase inhibitory activities of Areca catechu L extracted with hexane, $CHCl_3$, ethyl acetate, butanol, and water were measured. The water fraction showed the highest extraction yield at 3.65% (w/w). The butanol, $CHCl_3$, water, and ethyl acetate fractions showed strong antioxidative activities at 81.6%, 87.1%, 88.0%, and 89.5%, respectively. The fibrinolytic activity was strong only in the ethyl acetate fraction at 0.84 plasmin units/ml. The 100-fold dilution of the water fraction had the strongest thrombin inhibitory activity at 59.2%. The 100-fold dilution of butanol fraction displayed the strongest ${\alpha}$-glucosidase inhibitory activity at 88.6%. In conclusion, the extracts of Areca catechu L hold promise for use in the development of biofunctional foods to prevent cardiovascular diseases.

당뇨 처방에 근거한 생약재의 α-Glucosidase 활성 저해 효과 및 이를 활용한 미백 소재 평가법 (Effect of Medicinal Herb Prepared through Traditional Antidiabetic Prescription on α-Glucosidase Activity and Evaluation Method for Anti-Melanogenesis Agents Using α-Glucosidase Activity)

  • 김미진;임경란;윤경섭
    • 한국식품영양과학회지
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    • 제44권7호
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    • pp.993-999
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    • 2015
  • 본 연구에서는 선정한 생약재 및 복합처방단의 ${\alpha}$-glucosidase 저해 활성을 알아보았으며, 이 방법이 미백 소재 스크리닝을 위한 유용한 평가법인지를 알아보았다. 한의학과 민간에서 당뇨의 개선 및 치료 효과가 우수하다고 알려진 생약재 및 처방 중 죽력, 귀전우, 적양, 연자육, 마인, 청심연자음의 ${\alpha}$-glucosidase 활성 저해 효과는 식후 혈당조절제인 acarbose와 비교하여 볼 때 우수한 효과를 나타내었다. 미백 효과가 알려진 연자육을 함유한 청심연자음 hydrolyzed EtOAc layer는 $100{\mu}g/mL$ 농도에서 약 50% 멜라닌 생성 저해 효과를 보였다. 또한 청심연자음 hydrolyzed EtOAc layer는 ${\alpha}$-glucosidase 활성 저해 효과가 우수하였으나 mushroom tyrosinase 활성 저해 효과는 나타나지 않았다. 이로써 청심연자음 hydrolyzed EtOAc layer는 ${\alpha}$-glucosidase 활성을 저해시켜 tyrosinase의 glycosylation을 저해함으로써 멜라닌 생성 억제 효과가 나타나는 것으로 생각된다. 이상의 결과로 볼 때 ${\alpha}$-glucosidase 활성 억제 효과가 있으면서 당뇨병에 효과가 있는 생약재들은 N-linked glycoprotein인 tyrosinase의 glycosylation을 저해하여 tyrosinase의 세포 내 이동이나 활성을 억제함으로써 멜라닌 생성을 억제할 것으로 사료되며, 본 연구에서 선정된 생약재들은 당뇨병 치료를 위한 목적뿐만 아니라 화장품에서 새로운 미백 소재로서의 활용가치가 있을 것으로 판단된다. 또한 미백에 효과가 있는 소재 스크리닝을 위해 현재 널리 사용되고 있는 mushroom tyrosinase 활성 저해 효과와 다른 접근 방법으로써 ${\alpha}$-glucosidase 활성 측정 방법도 하나의 평가법으로 유용할 것으로 생각된다.

가시오갈피(Eleutherococcus senticosus) 잎으로부터 α-Glucosidase의 저해 활성 물질, Hyperoside와 Isoquercetin의 분리 및 구조·동정 (Isolation and Identification of α-Glucosidase Inhibitory Compounds, Hyperoside, and Isoquercetin from Eleutherococcus senticosus Leaves)

  • 이기연;홍수영;정혜정;이재형;임상현;허남기;김성문;김희연
    • 한국식품영양과학회지
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    • 제43권12호
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    • pp.1858-1864
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    • 2014
  • 가시오갈피 잎에 함유된 ${\alpha}$-glucosidase의 저해 활성 물질의 분리를 위하여 가시오갈피 잎 80% 에탄올 추출물을 극성유기 용매를 사용하여 순차 분획하고 각 분획층을 ${\alpha}$-glucosidase의 저해 활성 효과를 측정한 결과, EtOAc 층이 68.05%로 가장 높은 저해 활성을 나타내었다. EtAOc 분획층을 MPLC를 이용하여 fractionation-directed isolation을 수행하고 최종적으로 ${\alpha}$-glucosidase 저해 활성이 93.60%로 가장 우수하게 나타난 EAHC 분획물을 얻었다. EAHC 분획물을 prep-LC/MS로 분석하여 EAHCA와 EAHCB로 분리 정제하였다. EAHCA 분획물의 화학구조를 구명하기 위하여 $^1H$-NMR, $^{13}C$-NMR로 분석한 결과, 분자량 464.38 g/mol, 화학구조식 $C_{21}H_{20}O_{12}$인 hyperoside로 확인되었다. EAHCB 분획물의 화학구조를 구명하기 위하여 $^1H$-NMR, $^{13}C$-NMR로 분석한 결과, 분자량 464.38 g/mol, 화학구조식 $C_{21}H_{20}O_{12}$인 isoquercetin으로 확인되었다. 본 연구 결과, 가시오갈피 잎으로부터 분리 동정된 hyperoside와 isoquercetin은 ${\alpha}$-glucosidase의 저해 활성 물질을 가진 화합물로 향후 혈당조절용 건강식품 또는 치료제 개발을 위한 물질로 활용될 수 있을 것으로 판단된다.

참두릅 잎의 Protein Tyrosine Phosphatase 1B와 α-Glucosidase 저해 활성 (Inhibitory Activity of Aralia elata Leaves on Protein Tyrosine Phosphatase 1B and α-Glucosidase)

  • 조윤숙;성수희;바크타 히만수 쿠마르;정희진;문경호;최재수
    • 생약학회지
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    • 제47권1호
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    • pp.29-37
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    • 2016
  • Anti-diabetic potential of the leaves of A. elata through the inhibitory activity on PTP1B and ${\alpha}$-glucosidase has not been reported. In this study, the EtOAc fraction of methanolic extract from the leaves of A. elata showed potent inhibitory activity against the PTP1B and ${\alpha}$-glucosidase with $IC_{50}$ value of $96.29{\pm}0.3$ and $264.71{\pm}14.87{\mu}g/mL$, respectively. Three known triterpenoids, oleanolic acid, oleanolic acid-28-O-${\beta}$-D-glucopyranoside and oleanolic acid-3-O-${\beta}$-D-glucopyranoside were isolated from the most active EtOAc fraction. We determined the chemical structure of these triterpenoids through comparisons of published nuclear magnetic resonance (NMR) spectroscopic data. Furthermore, we screened these triterpenoids for their ability to inhibit PTP1B and ${\alpha}$-glucosidase over a range of concentrations ($12.5-50{\mu}M$). All three terpenoids significantly inhibited PTP1B in a concentration dependent manner and oleanolic acid effectively inhibited ${\alpha}$-glucosidase. In addition, these compounds revealed potent inhibitory activity with negative binding energies toward PTP1B, showing high affinity and tight binding capacity in the molecular docking studies. Therefore, the results of the present study clearly demonstrate that A. elata leaves and its triterpenoid constituents might be beneficial in the prevention or treatment of diabetic disease.

발아에 따른 콩류의 식후 혈당 상승 억제효능과 항산화 활성 (Enhancement of the Anti-hyperglycemic and Antioxidant Activities of Five Selected Beans by the Germination Process)

  • 조차영;최황용;조성훈;하경수;정지상;장해동;권영인
    • 한국식품영양학회지
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    • 제25권2호
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    • pp.246-252
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    • 2012
  • After a mixed carbohydrate diet, inhibition of ${\alpha}$-amylase and ${\alpha}$-glucosidase involved in the digestion and absorption of carbohydrates can significantly decrease the postprandial increase of blood glucose level. In the course of screening these useful enzyme inhibitors, we selected five kinds of bean, using an in-vitro enzyme inhibition assay method. To evaluate the effect of germination process on the functionality of the bean, we investigated the inhibitory activities of the water extracts of non-germinated bean and germinated bean against ${\alpha}$-amylase and ${\alpha}$-glucosidase, relevant to postprandial hyperglycemia. We also investigated the oxygen radical absorbance capacity(ORAC), total phenolics content, and postprandial blood glucose lowering effect in rats(Sprague-Dawley rat model). Most germinated beans showed significantly higher ${\alpha}$-glucosidase inhibitory activity, compared with non-germinated beans. Among germinated beans, Glycine max had the highest ${\alpha}$-glucosidase inhibitory activity(53.3%). The water extract of germinated Phaseolus vulgaris L. had the highest ${\alpha}$-amylase inhibitory activity(95.1%), followed by Glycine max(58.7%), and Glycine max L. Merr(54.1%). Furthermore, the five germinated beans also showed high antioxidant activities in ORAC assay. Results suggested that the germination process may improve and enhance the anti-hyperglycemia potential and antioxidant activity of the bean.

Hypoglycemic Effect of Padina arborescens Extract in Streptozotocin-induced Diabetic Mice

  • Park, Mi Hwa;Han, Ji Sook
    • Preventive Nutrition and Food Science
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    • 제17권4호
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    • pp.239-244
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    • 2012
  • This study investigated the hypoglycemic effect of the Padina arborescens extract in STZ-induced diabetic mice. Freeze-dried Padina arborescens were extracted with 80% methanol and concentrated for use in this study. The hypoglycemic effect was determined by inhibitory activities against ${\alpha}$-glucosidase and ${\alpha}$-amylase as well as the alleviation of postprandial blood glucose level. Padina arborescens extracts showed higher inhibitory activities than acarbose, a positive control against ${\alpha}$-glucosidase and ${\alpha}$-amylase. The $IC_{50}$ values of Padina arborescens extracts against ${\alpha}$-glucosidase and ${\alpha}$-amylase were 0.26 and 0.23 mg/mL, respectively, which evidenced as more effective than observed with acarbose. The increase of postprandial blood glucose levels were significantly suppressed in the Padina arborescens extract administered group than the control group in the streptozotocin induced diabetic mice. Furthermore, the area under the curve (AUC) was significantly lowered via Padina arborescens extract administration in diabetic mice (p 0.05). These results indicated that the Padina arborescens extract might be used as an inhibitor of ${\alpha}$-glucosidase and ${\alpha}$-amylase and delay absorption of dietary carbohydrates.

The activity of ${\alpha}$-amylase and ${\alpha}$-glucosidase as anti-diabetic function

  • Kim, Misook;Kim, Eunji;Kwak, Han Sub;Jeong, Yoonhwa
    • Nutrition Research and Practice
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    • 제8권5호
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    • pp.602-606
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    • 2014
  • BACKGROUND/OBJECTIVES: We investigated total 26 ingredients of Saengshik which will be commercially produced as an anti-diabetic dietary supplement. SUBJECTS/METHODS: Thirteen vegetables, nine cereals, three legumes and one seed were extracted with aqueous ethanol for 2 h at $60^{\circ}C$, and evaluated for their inhibitory effects against ${\alpha}$-amylase and ${\alpha}$-glucosidase and for total phenolic and flavonoid contents. RESULTS: All ingredients inhibited ${\alpha}$-amylase activity except cabbage. Strong inhibitory activity of ${\alpha}$-amylase was observed in leek, black rice, angelica and barley compared with acarbose as a positive control. Stronger inhibition of ${\alpha}$-glucosidase activity was found in small water dropwort, radish leaves, sorghum and cabbage than acarbose. All Saengshik ingredients suppressed ${\alpha}$-glucosidase activity in the range of 0.3-60.5%. Most ingredients contained total phenols which were in the range of 1.2-229.4 mg gallic acid equivalent/g dried extract. But, total phenolic contents were not observed in carrot, pumpkin and radish. All ingredients contained flavonoid in the range of 11.6-380.7 mg catechin equivalent/g dried extract. CONCLUSIONS: Our results demonstrate that Saengshik containing these ingredients would be an effective dietary supplement for diabetes.